252357-43-0Relevant articles and documents
A designed P1 cysteine mimetic for covalent and non-covalent inhibitors of HCV NS3 protease.
Narjes, Frank,Koehler, Konrad F,Koch, Uwe,Gerlach, Benjamin,Colarusso, Stefania,Steinkuehler, Christian,Brunetti, Mirko,Altamura, Sergio,De Francesco, Raffaele,Matassa, Victor G
, p. 701 - 704 (2002)
The difluoromethyl group was designed by computational chemistry methods as a mimetic of the canonical P1 cysteine thiol for inhibitors of the hepatitis C virus NS3 protease. This modification led to the development of competitive, non-covalent inhibitor 4 (K(i) 30 nM) and reversible covalent inhibitors (6, K(i) 0.5 nM; and 8 K*(i) 10 pM).